PF-5274857 (hydrochloride)
PF-5274857 hydrochloride is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 hydrochloride has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway[1].
Product Specifications
CAS Number
1613439-62-5
UNSPSC
12352005
Target
Smo
Type
Reference compound
Related Pathways
Stem Cell/Wnt
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/pf-5274857-hydrochloride.html
Solubility
10 mM in DMSO
Smiles
O=C(N1CCN(C2=NC=C(Cl)C(C3=NC=C(C)C=C3C)=C2)CC1)CCS(=O)(C)=O.Cl
Molecular Formula
C20H26Cl2N4O3S
Molecular Weight
473.42
References & Citations
[1]Rohner A, et, al. Effective targeting of Hedgehog signaling in a medulloblastoma model with PF-5274857, a potent and selective Smoothened antagonist that penetrates the blood-brain barrier. Mol Cancer Ther. 2012 Jan;11 (1) :57-65.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Frequently Asked Questions
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